相信你的直觉：肠道限制药物的策略与技巧。
Trust Your Gut: Strategies and Tactics for Intestinally Restricted Drugs.
作者信息
Dorel Ruth, Wong Alice R, Crawford James J
机构信息
Genentech, Inc., South San Francisco, California 94080, United States.
出版信息
ACS Med Chem Lett. 2023 Feb 22;14(3):233-243. doi: 10.1021/acsmedchemlett.3c00001. eCollection 2023 Mar 9.
Abstract
Non-absorbable small-molecule drugs targeted to the gut represent an alternative approach to safe, non-systemic therapeutics. Such drugs remain confined to the gastrointestinal tract upon oral dosing by virtue of their limited passive permeability, increasing the local concentration at the site of action while minimizing exposure elsewhere in the body. Herein we review the latest advances in the field of gut-restricted therapeutics, highlighting the different strategies and tactics that medicinal chemists have employed in pursuit of drugs with minimal intestinal absorption.
摘要
靶向肠道的不可吸收小分子药物是一种实现安全、非全身性治疗的替代方法。这类药物口服给药后，由于其被动通透性有限，会局限于胃肠道内，从而提高作用部位的局部浓度，同时将身体其他部位的暴露降至最低。在此，我们综述肠道限制疗法领域的最新进展，重点介绍药物化学家为研发肠道吸收最少的药物所采用的不同策略和方法。
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